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Application of 5- (3'-Indolyl)-oxazole compound in preparing drugs for inhibiting mycobacterium tuberculosis and curing tuberculosis

A technology of Mycobacterium tuberculosis and oxazoles, which is applied in the direction of antibacterial drugs, etc., can solve the problems that are difficult to penetrate the cell wall and limit clinical application.

Inactive Publication Date: 2011-04-06
MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Coumarin drugs such as novobiocin are DNA gyrase inhibitors acting on the B subunit, but their clinical application is limited due to their difficulty in penetrating the cell wall

Method used

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  • Application of 5- (3'-Indolyl)-oxazole compound in preparing drugs for inhibiting mycobacterium tuberculosis and curing tuberculosis
  • Application of 5- (3'-Indolyl)-oxazole compound in preparing drugs for inhibiting mycobacterium tuberculosis and curing tuberculosis
  • Application of 5- (3'-Indolyl)-oxazole compound in preparing drugs for inhibiting mycobacterium tuberculosis and curing tuberculosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Embodiment 1. The fermentation culture of Streptomyces 9792

[0037] 1) Composition of medium

[0038] a. ISP2 slant medium: malt extract 1.0%, yeast extract 0.4%, glucose 0.4%, agar 1.2%, pH 7.0.

[0039] b. Primary and secondary seed medium: glucose 0.5%, malt extract 1.0%, yeast extract 0.5%, cottonseed cake powder 1.0%, KH 2 PO 4 0.05%, (NH4) 2 SO 4 0.5%, CaCO 3 0.3%, NaCl0.1%, pH7.2.

[0040] 2) Culture method

[0041] Cultivate Streptomyces 9792 on the ISP2 slant medium at 28°C for one day; inoculate the slant of the strain on the primary seed medium and cultivate it at 28°C for 2 days; transfer the primary seed medium to the secondary seed at 5% The culture medium was cultured at 28°C for 4 days, and the fermentation broth was harvested.

Embodiment 2

[0042] The separation and purification of embodiment 2.2-methyl-5-(3'-indolyl) oxazole and 2-ethyl-5-(3'-indolyl) oxazole

[0043]25 liters of Streptomyces 9792 fermentation broth was filtered, and the filtrate was adsorbed with DiaionHP20 macroporous adsorption resin at a volume ratio of 10:1, followed by a gradient of water, 20%, 50%, 80%, and 100% acetone of two column volumes For elution, the activity of each eluate was followed by disc agar diffusion. After testing, the active component is in the 80% acetone eluent, and the diameter of its bacteriostatic zone is about 28mm. The fraction eluted with 80% acetone was collected and concentrated under reduced pressure to obtain 6.8 g of brown-red crude product. Weigh 1 gram of crude product, put it on a 30mmI.D.×400mm ODS column, and elute with 30%, 60%, 80%, and 100% methanol-water solution gradient respectively, collect and measure activity in sections, and the active components are washed in 60% methanol During dehydratio...

Embodiment 3

[0044] Physical and chemical properties and spectral characteristics of embodiment 3.2-methyl-5-(3'-indolyl) oxazole and 2-ethyl-5-(3'-indolyl) oxazole

[0045] 2-Methyl-5-(3'-indolyl)oxazole is a white powder, easily soluble in methanol, ethyl acetate, chloroform and other organic solvents, For 224, 265, 282 (sh), 298 (sh). Molecular weight is 198, molecular formula C 12 h 10 N 2 O.

[0046] 2-Ethyl-5-(3'-indolyl)oxazole is a white powder, easily soluble in methanol, ethyl acetate, chloroform and other organic solvents, For 224, 265, 282 (sh), 298 (sh). The molecular weight is 212, and the molecular formula is C 13 h 12 N 2 O.

[0047]

[0048] 2-Methyl-5-(3'-indolyl)oxazole R=CH 3

[0049] 2-Ethyl-5-(3'-indolyl)oxazole R=CH 2 CH 3

[0050] Table 1 H and C spectra data of 2-methyl-5-(3’-indolyl)oxazole and 2-ethyl-5-(3’-indolyl)oxazole

[0051]

[0052] a: 500M Hz in CD3OD b: 125M Hz in CD3OD c: 400M Hz in DMSO-d6 d: 100MHz in DMSO-d6

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Abstract

The invention relates to an application of a 5- (3'-Indolyl)-oxazole compound as shown in formula I in preparing drugs for inhibiting mycobacterium tuberculosis and curing tuberculosis, and in the formula I, R represents a liner C2-C10 saturated alkane substituent group or a C2-C10 saturated alkane substituent group containing branched chains, and R is preferably methyl or ethyl. A microplate Alamar Blue method is used to test the antibacterial effect of the 5- (3'-Indolyl)-oxazole compound on mycobacterium tuberculosis H37Rv, which shows that the compound has mycobacterium tuberculosis resistance.

Description

technical field [0001] The present invention relates to the compound described in the following formula 1, 5-(3'-indolyl)-oxazole compound is used in the preparation of the purposes of inhibiting Mycobacterium tuberculosis and treating tuberculosis. [0002] [0003] where R stands for C 2 ~C 10 straight-chain or branched-chain saturated alkane substituents. Background technique [0004] Tuberculosis (Tuberculosis) is a chronic infectious disease caused by Mycobacterium tuberculosis infection, which seriously endangers human life and health. In recent years, tuberculosis has made a comeback around the world, and now one-third of the world's population has been infected with Mycobacterium tuberculosis. According to the World Health Organization, there were 9.27 million new cases of tuberculosis in the world in 2007, higher than the 9.24 million cases in 2006, 8.3 million cases in 2000 and 6.6 million cases in 1990. In 2007, 1.77 million people died of tuberculosis in t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/422A61P31/06
Inventor 司书毅姜威肖春玲樊秀勇郝雪秦刘伟张月琴余利岩
Owner MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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